一种新的三嗪类抗锥虫药:SIPI-1029及其类似物的合成和抗原虫作用

合成了1,2-二氢-2,2-二甲基-4,6-二氨基-1-(ω-卤代烷氧基)-s-三嗪类和O,O’-双(4,6-二氨基-1,2-二氢-2,2-二取付-s-三嗪-1-基)烷烃二醇两类化合物,它们大多有较好的体内抗疟原虫(Plasmodium berghei)作用,化合物IIc～e对用伊氏锥虫(Trypanosoma evansi)感染的小鼠,有较好的作用,经深入的药理、毒理和药代动力学以及疗效等研究,化合物IIe(SIPI-1029,T-46)被证明是一高效、低毒并有较长的血药半衰期的抗锥虫新药。     

DDAVP enhances platelet adherence and platelet aggregate growth on human artery subendothelium

The effect of intravenous 1-deamino (8-D-arginine)vasopressin (DDAVP) administration on platelet interaction with human artery subendothelium was investigated with flowing blood from five normal individuals and 12 patients with von Willebrand's disease (vWD). Three of the patients were diagnosed as vWD subtype I, four as subtype IIa, and five as subtype IIb. DDAVP administration to normals enhanced platelet adherence, in parallel with increasing plasma levels of factor VIII- related antigen ( FVIIIR :Ag) and ristocetin cofactor activity ( FVIIIR :RCF). Platelet aggregate formation was transiently increased within 90 minutes. Platelet adherence in patient blood before DDAVP infusion was subnormal. In patients with subtype I, administration of DDAVP normalized the bleeding time, enhanced the platelet adherence, and transiently improved the platelet aggregate formation. The platelet adherence was more corrected than would have been expected on the basis of the FVIIIR :Ag and FVIIIR :RCF levels. In patients with subtype IIa, infusion of DDAVP increased the FVIIIR :Ag levels approximately threefold, without affecting the FVIIIR :RCF levels, and in only two of four patients was a transiently enhanced platelet adherence with a corresponding shortening of the bleeding time observed. In patients with subtype IIb, administration of DDAVP increased the FVIIIR :Ag levels about threefold and the FVIIIR :RCF levels five to tenfold, but decreased the platelet adherence significantly. The bleeding time values were not normalized. A close association between the bleeding time values and corresponding platelet adherence values before and after DDAVP infusion was observed. Normalization of the bleeding time was paralleled with normalization of platelet adherence. We conclude that DDAVP improves the primary hemostasis by causing enhanced FVIII- vWF-mediated platelet adherence. DDAVP has little or no effect on the bleeding time in patients with subtype IIa and subtype IIb, because the platelet adherence is not normalized.     

螺内酯在慢性充血性心力衰竭治疗中的应用

1临床资料2003-01/2004-12,我院慢性充血性心力衰竭(心衰)住院患者238例中,使用螺内酯者185(男127,女58)例,使用率为77.7%(185/238),年龄32~96(平均61.2)岁.     

Factors affecting lymph node yield from patients undergoing colectomy for cancer

Purpose  

Lymph node (LN) yield is a critical component of colon cancer staging and is often a surrogate for quality assessment in surgery. We investigated the impact of pathologists’ training on LN harvest.